Effect of flumazenil on GABA^sub A^ receptors in isolated rat hippocampal neurons
Using whole cell patch-clamp recordings from pyramidal cells acutely dissociated from rat hippocampal slices, Ro-15 1788 (flumazenil, FLU) was shown to enhance the GABAA-receptor mediated currents evoked by application of gamma-aminobutyric acid (GABA) and to antagonize the enhancing effect of the b...
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| Published in: | Neurochemical research Vol. 27; no. 12; p. 1605 |
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| Main Authors: | , , |
| Format: | Journal Article |
| Language: | English |
| Published: |
New York
Springer Nature B.V
01-12-2002
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| Online Access: | Get full text |
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| Summary: | Using whole cell patch-clamp recordings from pyramidal cells acutely dissociated from rat hippocampal slices, Ro-15 1788 (flumazenil, FLU) was shown to enhance the GABAA-receptor mediated currents evoked by application of gamma-aminobutyric acid (GABA) and to antagonize the enhancing effect of the benzodiazepine agonist flurazepam (FZP) on the GABAA response. Both FLU and FZP increased the peak and the steady-state components of the responses and accelerated the current decay. This suggests that both agents act via a common mechanism on GABA transmission. It is concluded that FLU possesses high affinity for the binding site, but low efficacy on the GABAA-benzodiazepine receptor. This suggests that FLU acts as a partial agonist on GABAA receptors. |
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| ISSN: | 0364-3190 1573-6903 |